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Nano liver target direction amphipathic nature block copolymers drug administration system and preparation

A technology of amphiphilic block and drug delivery system, which is applied in the field of nano-liver targeted amphiphilic block copolymer drug delivery system, can solve the problems of poor targeting and low bioavailability of anticancer drugs, and achieve maintenance The effect of drug activity, increasing curative effect and reducing adverse reactions

Inactive Publication Date: 2008-08-27
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And it can achieve highly targeted and sustained-release drug delivery to the liver through injection, which can solve the shortcomings of poor targeting and low bioavailability of current anticancer drugs, and improve the quality of life of patients

Method used

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  • Nano liver target direction amphipathic nature block copolymers drug administration system and preparation
  • Nano liver target direction amphipathic nature block copolymers drug administration system and preparation
  • Nano liver target direction amphipathic nature block copolymers drug administration system and preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Example 1: Preparation of double-terminal amino polyethylene glycol modified by liver targeting compound

[0075] 1.1 Glycyrrhetinic acid-polyethylene glycol 2000 (GA-PEG 2000 -NH 2 ) preparation

[0076] Dissolve 10mmol of glycyrrhetinic acid in 35mL of tetrahydrofuran, add 2.54g (12.3mmol) of DCC under cooling, stir for 0.5h, add 1.42g (12.3mmol) of NHS, continue stirring for 15h, filter, anhydrous ether precipitates, collect white solid, Vacuum drying to obtain glycyrrhetinic acid active ester.

[0077] Dissolve 5 mmol of glycyrrhetinic acid active ester and 10 mmol of double-terminated amino polyethylene glycol (molecular weight: 2000) in N,N'-dimethylformamide, react at 40°C for 15 h, precipitate with ether, collect the solid, and dry in vacuo. The product was passed through a Sephadex G-25 column and freeze-dried. Glycyrrhetinic acid modified aminopolyethylene glycol 2000 , denoted as GA-PEG 2000 -NH2 .

[0078] 1.2 Glycyrrhetinic acid-polyethylene glycol ...

Embodiment 2

[0086] Example 2: Preparation of liver targeting amphiphilic block copolymer drug carrier material

[0087] 2.1 Glycyrrhetinic acid-polyethylene glycol 3400 - Polybenzyl glutamate (GA-PEG 3400 -PBLG) preparation, the molar ratio is GA-PEG 3400 -NH 2 : benzyl glutamate nitrogen carboxylic acid anhydride monomer = 1:15

[0088] Weigh 1mmol glycyrrhetinic acid modified aminopolyethylene glycol 3400 (GA-PEG 3400 -NH 2 ), 15mmol benzyl glutamate nitrogen carboxylic acid anhydride monomer in a reaction flask, add 120mL N, N'-dimethylformamide, and stir at room temperature under nitrogen protection for 48h. Precipitate with anhydrous ether, filter, and dry to obtain a white solid to obtain glycyrrhetinic acid-polyethylene glycol 3400 -Polybenzyl glutamate, denoted as GA-PEG 3400 -PBLG.

[0089] 2.2 Glycyrrhetinic acid-polyethylene glycol 2000 - Polybenzyl aspartate (GA-PEG 2000 - the preparation of PBLA), molar ratio is GA-PEG 2000 -NH 2 : benzyl aspartate nitrogen carbo...

Embodiment 3

[0102] Example 3: Preparation of nano-liver targeting amphiphilic block copolymer drug delivery system

[0103] 3.1 Preparation of glycyrrhetinic acid-polyethylene glycol 3400 -Nano-liver targeted drug delivery system with polybenzyl glutamate as carrier

[0104] Under magnetic stirring at room temperature, mix 20mg doxorubicin and 30mg glycyrrhetinic acid-polyethylene glycol prepared in Example 2.1 3400 -Polybenzyl glutamate was dissolved in 20 mL of N,N'-dimethylformamide. The system was transferred to a dialysis bag and dialyzed with 5 L of distilled water for 2 days to obtain a doxorubicin-embedded liver-targeted nanoparticle solution, namely a drug delivery system. The nanoparticle morphology and particle size were analyzed by transmission electron microscopy, and the results are shown in the appendix figure 2 , particle size 140 ~ 160nm, the particles are round and spherical, uniform in size.

[0105] 3.2 Preparation of glycyrrhetinic acid-polyethylene glycol 2000 ...

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Abstract

The invention relates to a drug delivery system of nanometer liver targeting amphiphilic block copolymer and a preparation method thereof. The nanometer liver targeting drug delivery system is obtained by adopting liver targeting amphiphilic block copolymer which can be biologically degraded and which has good biocompatibility as the carrier material and embedding drugs for treating liver diseases by a solvent dialysis method or a solvent evaporation method; the weight ratio of the carrier material to the drug is 1:0.1 to 1.2. The drug delivery system has the advantages of simple operation, mild condition and cheap raw material; the prepared drug delivery system has good biocompatibility and both effects of active targeting and passive targeting, and can realize high targeting and sustained release drug delivery to the liver by means of injection, thus solving the defects of bad targeting and low bioavailability of present anticancer drugs and improving the life quality of patients, with broad application prospects.

Description

technical field [0001] The invention relates to a biodegradable nano-liver targeting amphiphilic block copolymer drug delivery system and a preparation method. The liver-targeting compound is modified onto the biodegradable and biocompatible amphiphilic block copolymer drug carrier, and the drug for the treatment of liver diseases is prepared by solvent dialysis or solvent evaporation to obtain nano-hepatic targeting compounds. Amphiphilic block copolymer drug delivery system. Background technique [0002] The liver is the largest detoxification organ in the human body. It plays a vital role in the regulation of human metabolism, blood coagulation, immunity and other functions. Therefore, liver lesions seriously endanger human health. my country is a high-incidence area of ​​liver cancer, and the number of liver cancer patients is about 300,000 every year, accounting for 45% of the global liver cancer deaths. At present, liver transplantation is the first treatment for liv...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K47/48A61K45/00A61K31/337A61K31/4745A61K31/704C07J63/00C08G65/48A61P1/16A61P35/00A61K47/59
Inventor 袁直黄微张闯年田秦韩亮刘通张跃陈跃
Owner NANKAI UNIV
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